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Preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity

A technology targeting liposomes and fatty acids, which is applied in the field of biomedicine and can solve the problems that ordinary liposomes do not have targeting properties

Inactive Publication Date: 2012-07-04
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Ordinary liposomes are not targeted

Method used

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  • Preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity
  • Preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1CH 3 (CH 2 ) 10 CO-Arg-Gly-Asp-OCH 2 (CH 2 ) 10 CH 3 preparation of

[0045] 1) Preparation of Boc-Arg(NO2)-Gly-OBzl

[0046] 1.59 g (5 mmol) Boc-Arg(NO2)-OH, 0.68 g (5 mmol) N-hydroxybenzotriazole (HOBt) were dissolved in anhydrous THF. 1.34 g (5.75 mmol) of anhydrous THF solution of dicyclohexylcarbodiimide (DCC) was added dropwise under ice bath, and stirred for 20 minutes under ice bath to obtain reaction solution (I). Suspend 1.69g (5.0mmol) TosOH·Gly-OBzl in an appropriate amount of anhydrous DMF under ice-cooling, then add a few drops of N-methylmorpholine (NMM) to adjust the pH to 7-8 to obtain the reaction solution (II) . Add the reaction solution (I) dropwise to the reaction solution (II) under ice bath, first stir under ice bath for 1 h, then stir at room temperature for 12 h, TLC (chloroform / methanol, 10:1) shows that Boc-Arg(NO2)-OH disappears , stop responding. Dicyclohexylurea (DCU) was filtered off, and the filtrate was blown off of D...

Embodiment 2

[0062] Embodiment 2. The preparation of epirubicin liposome (2)

[0063] Prepared by ammonium sulfate gradient method. Take an appropriate amount of phospholipids and cholesterol into a round bottom flask and dissolve them in chloroform, and remove the solvent by rotary evaporation, forming a transparent film on the bottle wall. 150mmol·L -1 (NH 4 ) 2 SO 4 The solution was added to the lipid film, and ultrasonically dispersed to obtain a blank liposome suspension. Put the blank liposome in the dialysis bag for dialysis 4-5 times, each time for about 10 hours, take out the dialysis liquid and place it in an eggplant bottle; in addition, accurately weigh an appropriate amount of epirubicin, dissolve it in water, and add this solution to Place the blank liposome suspension in a hot water bath and shake it from time to time. After taking out from the hot water bath, the epirubicin liposome is obtained.

[0064] Particle size 150~250nm, Zeta-Potential-20~-40mV.

Embodiment 3

[0065] Example 3. Containing CH in the membrane material 3 (CH 2 ) 10 CO-GGD-OCH 2 (CH 2 ) 10 CH 3 Preparation of epirubicin liposomes (3)

[0066] The dosage of each component: epirubicin 2-8%; natural lecithin, cholesterol and CH 3 (CH 2 ) 10 CO-GGD-OCH 2 (CH 2 ) 10 CH 3 The mixture 90-97%, in this mixture, natural lecithin 70-80% (mass percentage), cholesterol 10-20% (mass percentage) and compound CH 3 (CH 2 ) 10 CO-GGD-OCH 2 (CH 2 ) 10 CH 3 3-10% (mass percentage).

[0067] Take phospholipids, cholesterol and CH 3 (CH 2 ) 10 CO-GGD-OCH 2 (CH 2 ) 10 CH 3 Dissolve in chloroform in a round-bottomed flask, remove the solvent by rotary evaporation, and form a transparent film on the bottle wall. 150mmol·L -1 (NH 4 ) 2 SO 4 The solution was added to the lipid film, and ultrasonically dispersed to obtain a blank liposome suspension. Place the blank liposome in the dialysis bag for dialysis 4-5 times, each time for about 10 hours, take out the dialy...

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Abstract

The invention discloses preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity. According to the invention, the conjugate has the following structural formula: CH3(CH2)nCO-Arg-Gly-Asp-OCH2(CH2)10CH3, wherein n is equal to 4-16. An anticancer medicine is introduced into the conjugate to obtain anticancer targeted liposome medicine; the liposome can increase the concentration of the anticancer medicine at a target position, reduce the toxic and side effects of the anticancer medicine at a non-target position, and improve the therapeutic index of the medicine.

Description

technical field [0001] The present invention relates to a targeted drug release carrier, in particular to a fatty acid-RGD-fatty alcohol-mediated targeted drug carrier and its construction method. The present invention also relates to the application of a drug carrier in the preparation of targeted anti-tumor drug liposomes, which belongs to biological field of medicine. Background technique [0002] The growth and metastasis of many malignant tumors are related to abnormal expression of integrins or changes in molecular structure. Integrins are a large family of transmembrane proteins, consisting of α and β subunits to form heterodimers. At present, it has been found that there are about 18 kinds of α, about 8 kinds of β, and at least 24 kinds of integrin forms of heterodimers. The progression of integrins in tumors may be dual: 1) In the early stage of tumorigenesis, the reduction of integrin expression can weaken the adhesion between tumor cells and basement membrane or...

Claims

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Application Information

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IPC IPC(8): C07K5/09C07K1/113A61K47/42A61K9/127A61K31/337A61K31/704A61P35/00
Inventor 崔国辉崔纯莹吴曼
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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